1. Protein Tyrosine Kinase/RTK
  2. Syk
  3. RO9021

RO9021 

Cat. No.: HY-16902 Purity: 98.89%
Handling Instructions

RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.

For research use only. We do not sell to patients.

RO9021 Chemical Structure

RO9021 Chemical Structure

CAS No. : 1446790-62-0

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1 mg USD 99 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

RO9021 is an orally bioavailable, novel ATP-competitive inhibitor of SYK, with an average IC50 of 5.6 nM.

IC50 & Target

IC50: 5.6 nM (SYK)

In Vitro

RO9021 is a highly selective SYK inhibitor with low S-scores of 0.003 for S(99) and 0.015 for S(90), indicating that SYK is the only kinase with 99% competition with RO9021 in a total of 392 tested kinases. RO9021 inhibits anti-IgM induced phosphorylation of BTK, PLCγ2, AKT and ERK, indicating that blockade of SYK kinase activity by RO9021 results in attenuation of BCR downstream signaling cascade. RO9021 selectively suppresses B-cell receptor signaling. RO9021 also displays a similar inhibitory potency (IC50=22.8±1.7 nM) in a FcεR-mediated mast cell activation and degranulation assay[1].

Molecular Weight

355.44

Formula

C₁₈H₂₅N₇O

CAS No.

1446790-62-0

SMILES

NC(C1=C(NC2=CC=C(C)C(C)=N2)C=C(N[[email protected]]3[[email protected]@H](N)CCCC3)N=N1)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.03 mg/mL (8.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8134 mL 14.0671 mL 28.1341 mL
5 mM 0.5627 mL 2.8134 mL 5.6268 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

The inhibitory potency to SYK is determined in a radiometric assay using inactive SYK kinase. Briefly, SYK protein is dephosphorylated by PTP1B phosphatase and then the reaction is initiated by the addition of substrate cocktail that contained 20 μM ATP, 0.025 μCi ATP-γ-33P and 10 μM biotinylated synthetic peptide. The reaction is carried out for 30 minutes and resulting 33P incorporation is determined by top counter.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Briefly, DBA1/J male mice are injected intradermally with 0.1 mL bovine type II collagen (100 μg) and complete Freund’s adjuvant followed by second immunization on day 21 with bovine type II collagen and incomplete Freund adjuvant. RO9021 is administered orally, randomized into different groups (14 mice/groups), every day for 14 days starting on the day after second immunization. Clinical arthritis scores (1 to 4) of individual paws are assessed and the arthritic index for each mouse is determined by adding the individual scores of all four paws. The level of cytokines in serum is determined by Luminex analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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RO9021
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HY-16902
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